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My CartCAS：155213-67-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 155213-67-5 |
| Name | Ritonavir |
| Molecular Formula | C37H48N6O5S2 |
| Molecular Weight | 720.94 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 208-127-9 |
| MDL | MFCD00927142 |
| SMILES | O=C(N[C@@H](CC1=CC=CC=C1)[C@H](C[C@H](CC2=CC=CC=C2)NC([C@H](C(C)C)NC(N(CC3=CSC(C(C)C)=N3)C)=O)=O)O)OCC4=CN=CS4 |
| Target Point | HIV Protease |
| Passage | Anti-infection |
| Background | Ritonavir is an inhibitor of HIV protease. |
| Biological Activity | Ritonavir是用于治疗HIV感染和AIDS的 HIV蛋白酶的抑制剂。[1-5] |
| In Vitro | 利托那韦是CYP3A4介导的睾酮6β-羟基化的抑制剂，平均Ki为19 nM，并且还抑制甲苯磺丁脲羟基化，IC50为4.2μM[1]。发现利托那韦是CYP3A介导的生物转化的有效抑制剂(硝苯地平氧化，IC50为0.07mM，17α-乙炔基雌二醇2-羟基化，IC50为2mM;特非那定羟基化，IC50为0.14mM)。利托那韦也是由CYP2D6(IC50 = 2.5 mM)和CYP2C9/10(IC50 = 8.0 mM)介导的反应的抑制剂[2]。利托那韦导致未感染的人PBMC培养物中细胞活力的增加。利托那韦显著降低PBMC对凋亡的易感性，其与较低水平的胱天蛋白酶-1表达相关，在膜联蛋白V染色中降低，并且在未感染的人PBMC培养物中降低胱天蛋白酶-3活性。利托那韦在无毒浓度下抑制PBMC和单核细胞以时间和剂量依赖性方式诱导肿瘤坏死因子(TNF)的产生[3]。利托那韦抑制p-糖蛋白介导的沙奎那韦挤压，IC50为0.2μM，表明利托那韦对p-糖蛋白具有高亲和力[4]。利托那韦有效抑制ABT-378的人肝微粒体代谢，Ki为13 nM。利托那韦联合ABT-378(比例为3：1和29：1)可抑制CYP3A(IC50 = 1.1和4.6μM)，尽管效果不如利托那韦(IC50 =0.14μM)[5]。 |
| Data Literature Source | [1]. Eagling VA，et al. Differential inhibition of cytochrome P450 isoforms by the protease inhibitors，ritonavir，saquinavir and indinavir. Br J Clin Pharmacol. 1997 Aug;44(2):190-4. [2]. Kumar GN，et al. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31. [3]. Weichold FF，et al. HIV-1 protease inhibitor ritonavir modulates susceptibility to apoptosis of uninfected T cells. J Hum Virol. 1999 Sep-Oct;2(5):261-9. [4]. Drewe J，et al. HIV protease inhibitor ritonavir: a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833. Biochem Pharmacol. 1999 May 15;57(10):1147-52. [5]. Kumar GN，et al. Potent inhibition of the cytochrome P-450 3A-mediated human liver microsomal metabolism of a novel HIV protease inhibitor by ritonavir: A positive drug-drug interaction. Drug Metab Dispos. 1999 Aug;27(8):902-8. |
| Unit | Bottle |
| Specification | 10mg 50mg 100mg |
Ritonavir是一种 HIV蛋白酶的抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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